产品说明书
FB23-2
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同义名 : | - |
| CAS号 : | 2243736-45-8 | |
| 货号 : | A1146406 | |
| 分子式 : | C18H15Cl2N3O3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 392.236 | |
| MDL号 : | MFCD32174281 | |
| 存储条件： |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 25 mg/mL(63.74 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The fat-mass and obesity-associated protein (FTO), a mRNA N6-methyladenosine (m6A) demethylase, is reported to promote leukemogenesis. FB23-2 is a potent and selective inhibitor of FTO, which binds directly to FTO and selectively inhibits FTO's m6A demethylase activity with an IC50 value of 2.6 μM. FB23-2 displayed significantly improved anti-proliferative activity on NB4 and MONOMAC6 cells with an IC50 of 0.8 – 1.5 μM and maintained inhibitory activity on FTO demethylation in vitro. FB23-2 substantially accelerated all-trans retinoic acid (ATRA)-induced myeloid differentiation in NB4 and MONOMAC6 cells in a dose-dependent manner. Furthermore, FB23-2 induced apoptosis and cell cycle arrest at G1 stage in AML cells. Collectively, these results suggest that FB23-2 exhibits FTO-dependent activity in AML cells. In a xeno-transplantation leukemic model, FB23-2 (2 mg/kg; intraperitoneally injected daily for 10 days) substantially delayed the onset of full-blown leukemic symptoms and significantly prolonged survival by almost doubling the median survival. Compared with the vehicle, FB23-2 treatment suppressed leukemia malignancy, including reduced splenomegaly and hepatomegaly, as well as the abundance of human AML cells in the recipient mice[1]. | ||
| 作用机制 | FB23-2 unambiguously shows an intramolecular hydrogen bond between the amino hydrogen and the carbonyl of hydroxamic acid[1]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.55mL 0.51mL 0.25mL |
12.75mL 2.55mL 1.27mL |
25.49mL 5.10mL 2.55mL |
| 参考文献 |
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